C-02 |
Catalog No.GC91442 |
C-02는 헥소키나제 억제제인 로니다민과 cereblon 리간드 탈리도마이드가 연결된 프로테올라이시스-타겟팅 카이메라(PROTAC)입니다.
Products are for research use only. Not for human use. We do not sell to patients.
Sample solution is provided at 25 µL, 10mM.
C-02 is a proteolysis-targeting chimera (PROTAC) composed of the hexokinase inhibitor lonidamine linked to the cereblon ligand thalidomide .1 It induces degradation of hexokinase 2 in 786-O and PANC-1 cells when used at a concentration of 20 µM. C-02 is cytotoxic to 786-O, 4T1, PANC-1, HGC-27, and MCF-7 cancer cells (IC50s = 34.07, 5.08, 31.53, 6.11, and 21.65 µM, respectively). It reduces the extracellular acidification rate (ECAR) and oxygen consumption rate (OCR) in 4T1 cells, indicating inhibition of glycolysis and mitochondrial damage, respectively, when used at a concentration of 20 µM. In vivo, C-02 (50 mg/kg) reduces tumor volume and induces intratumoral cytokine accumulation and pyroptosis in a 4T1 murine mammary carcinoma model.
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